Page last updated: 2024-10-24

nociceptin receptor activity

Definition

Target type: molecularfunction

Combining with the peptide nociceptin, and transmitting the signal across the membrane by activating an associated G-protein. [GOC:bf, GOC:mah, PMID:18670432]

Nociceptin receptor activity is a molecular function that involves the binding of nociceptin, a neuropeptide, to its specific receptor, the nociceptin/orphanin FQ receptor (NOP receptor). This binding initiates a signaling cascade within the cell, leading to various physiological effects.

The NOP receptor is a G protein-coupled receptor (GPCR) belonging to the opioid receptor family. Upon nociceptin binding, the receptor undergoes conformational changes, activating associated G proteins. These G proteins, primarily of the Gαi/o subtype, trigger intracellular signaling pathways.

One primary pathway involves the inhibition of adenylyl cyclase, an enzyme responsible for the production of cyclic adenosine monophosphate (cAMP). Decreased cAMP levels can lead to the modulation of ion channels, including potassium channels, and influence neuronal excitability.

Another important pathway involves the activation of mitogen-activated protein kinases (MAPKs), such as extracellular signal-regulated kinases (ERK) and p38 MAPK. MAPK signaling plays a role in various cellular processes, including gene expression, cell growth, and differentiation.

Nociceptin receptor activity is implicated in a wide range of physiological functions, including pain modulation, anxiety, reward, and appetite regulation. It is believed to contribute to the analgesic effects of nociceptin, while also potentially playing a role in the development of addiction.

The precise molecular mechanisms underlying nociceptin receptor activity are still under investigation. However, ongoing research continues to unravel the intricate signaling pathways and physiological consequences associated with this important molecular function.'
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Proteins (1)

ProteinDefinitionTaxonomy
Nociceptin receptorA nociceptin receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41146]Homo sapiens (human)

Compounds (21)

CompoundDefinitionClassesRoles
fluspirileneFluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.diarylmethane
loperamideloperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.

Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
atomoxetineatomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.aromatic ether;
secondary amino compound;
toluenes
adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
u 69593U 69593: selective ligand for opioid K-receptor

U69593 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of phenylacetic acid and the secodary amino group of (5R,7S,8S)-N-methyl-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-amine.
monocarboxylic acid amide;
N-alkylpyrrolidine;
organic heterobicyclic compound;
oxaspiro compound
anti-inflammatory agent;
diuretic;
kappa-opioid receptor agonist
j 113397J 113397: an opioid receptor-like 1 (ORL1), orphanin FQ, and nociceptin receptor antagonist; structure in first source
n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamideN-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide: a nociceptin antagonist; structure in first sourceaminoquinoline
naltrexonenaltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.

Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound
antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
enkephalin, ala(2)-mephe(4)-gly(5)-peptide
norbinaltorphiminenorbinaltorphimine: kappa opiate receptor antagonist; structure given in first sourceisoquinolines
dermorphindermorphin: opiate-like peptide present in amphibian skinoligopeptide
naltrindolenaltrindole: delta opioid receptor antagonistisoquinolines
pmx 53
camostat4-hydroxyatomoxetine: an atomoxetine metabolite; structure in first sourcearomatic ether;
phenols
ro 64-6198Ro 64-6198: an orphanin FQ/nociceptin receptor agonist; structure in first source
sr 14150SR 14150: mixed NOP and mu-opioid receptor ligand and antinociceptive; structure in first source
sb-612111
naluzotannaluzotan: an antidepressant and anti-anxiety agent; structure in first source
cebranopadol
a 803467A 803467: an Nav1.8 sodium channel blocker; structure in first source
nociceptinorganic molecular entity;
polypeptide
human metabolite;
rat metabolite
1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3R)-3-piperidinyl)-1H-benzimidazole: anxiolytic agent; structure in first source